A 61603 hydrobromide
Potent α-adrenoceptor agonist that is at least 35-fold more potent at α1A than at α1B or α1D sites. Induces dose response increases in spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nmol/L). Also available as part of the α1-Adrenoceptor Tocriset™.
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 50 mM in water|
References are publications that support the biological activity of the product.
Knepper et al (1995) A-61603, a potent α1-adrenergic receptor agonist, selective for the α1A receptor subtype. J.Pharmacol.Exp.Ther. 274 97 PMID: 7616455
Luo et al (2007) Receptor subtype involved in α1A-adrenergic receptor-mediated Ca2+ signaling in cardiomyocytes. Acta.Pharmacol.Sin. 28 968 PMID: 17588332
Meyer et al (1996) Synthesis and in vitro characterisation of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective α1A receptor agonist. J.Med.Chem. 39 4116 PMID: 8831777
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Keywords: A 61603 hydrobromide, A 61603 hydrobromide supplier, α1A-adrenoceptor, alpha1A-adrenoceptor, agonists, α1a-adrenergic, alpha1a-adrenergic, a1a-adrenergic, a1a-adrenoceptor, Receptors, A61603, hydrobromide, α1a, Adrenergic, Alpha-1, 1052, Tocris Bioscience
12 Citations for A 61603 hydrobromide
Citations are publications that use Tocris products. Selected citations for A 61603 hydrobromide include:
O-Uchi et al (2008) Interaction of α1-adrenoceptor subtypes with different G proteins induces opposite effects on cardiac L-type Ca2+ channel. PLoS One 102 1378 PMID: 18467629
Montgomery (2017) An Alpha-1A Adrenergic Receptor Agonist Prevents Acute Doxorubicin Cardiomyopathy in Male Mice. Plos One 12 e0168409 PMID: 28081170
Dash et al (2011) A molecular MRI probe to detect treatment of cardiac apoptosis in vivo. Magn Reson Med 66 1152 PMID: 21360750
Treen et al (2016) Divergent regulation of ER and kiss genes by 17 beta -estradiol in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217 PMID: 26726951
Desir and Peixoto (2014) Renalase in hypertension and kidney disease. Circ Res 29 42604 PMID: 24137013
Thomas et al (2016) The α-1A Adrenergic Receptor in the Rabbit Heart. Nephrol Dial Transplant 11 e0155238 PMID: 27258143
Jensen et al (2010) Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells. Naunyn Schmiedebergs Arch Pharmacol 382 475 PMID: 20857090
Thomas et al (2016) A Myocardial Slice Culture Model Reveals Alpha-1A-Adrenergic Receptor Signaling in the Human Heart. JACC Basic Transl Sci 1 155 PMID: 27453955
Copik et al (2015) Isoproterenol acts as a biased agonist of the α-1A-adrenoceptor that selectively activates the MAPK/ERK pathway. PLoS One 10 e0115701 PMID: 25606852
Amirak et al (2013) p90 ribosomal S6 kinases play a significant role in early gene regulation in the cardiomyocyte response to G(q)-protein-coupled receptor stimuli, endothelin-1 and α(1)-adrenergic receptor agonists. Biochem J 450 351 PMID: 23215897
Rokosh and Simpson (2002) Knockout of the alpha 1A/C-adrenergic receptor subtype: the alpha 1A/C is expressed in resistance arteries and is required to maintain arterial blood pressure. Proc Natl Acad Sci U S A 99 9474 PMID: 12093905
Jensen et al (2009) The α-1D Is the predominant α-1-adrenergic receptor subtype in human epicardial coronary arteries. PLoS One 54 1137 PMID: 19761933
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A61603 was used to treat H9C2 for 24hours, works well as intended.
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.